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Topical compositions of urea and ammonium lactate

a technology of ammonium lactate and composition, which is applied in the field of topical compositions containing high concentrations of urea and ammonium lactate, can solve the problems of many disadvantages of preparation, no additive hydrating effect, and high concentration of urea in topical formulations, and achieves stable and efficient effects

Inactive Publication Date: 2007-11-01
AGIS INDUSTRIES (1983) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides a stable and efficient pharmaceutical, cosmetic, or cosmeceutical composition for the treatment of various dermatological disorders such as dry skin, scalp, and acne. The composition contains urea and / or a derivative thereof, an alpha-hydroxy acid and / or a salt thereof, and a carrier. The concentration of urea and / or the derivative thereof is greater than 5 weight percentages of the composition, and the concentration of ammonium lactate is greater than 5 weight percentages of the composition. The composition can be in the form of a cream, ointment, paste, gel, lotion, milk, suspension, aerosol, spray, foam, shampoo, hair conditioner, serum, swab, pad, or soap. The composition can also contain additional active ingredients such as antibiotic agents, antimicrobial agents, anti-acne agents, antifungal agents, anti-inflammatory agents, steroidal anti-inflammatory agents, non-steroidal anti-inflammatory agents, anesthetic agents, antipruriginous agents, antioxidants, chemotherapeutic agents, antidepressants, antihistamines, vitamins, hormones, and antidandruff agents. The composition has a pH value of about 5.0 to about 8.0."

Problems solved by technology

However, these commercial preparations are disadvantageous as they are characterized by low absorption and high stickiness.
Although lactic acid is a known hydrating agent, its concentration in this preparation is relatively low and therefore provides no additive hydrating effect.
Nevertheless, topical formulations containing high concentrations of urea suffer many disadvantages.
Such a pH value is much higher than that of the natural skin (about 5.5), and may therefore cause irritations when applied.
Moreover, topical application of formulations that contain high urea concentrations are typically associated with an unpleasant odor of ammonia, formed by the decomposition of urea, stickiness, and white stains that remain on the skin and clothing after the evaporation of the solvent.
Hence, although both urea and ammonium lactate have been shown to act as highly efficient hydrating agents, and thus may serve as potent agents for treating dry skin conditions, the presently available topical formulations that comprise high concentrations of either urea or ammonium lactate suffer severe limitations.
U.S. Pat. No. 5,679,324 therefore teaches compositions that may optionally comprise urea or ammonium lactate and fails to teach compositions in which these substances are combined as active ingredients for the treatment of dry skin or scalp.
Hence, the composition disclosed in this patent application comprises low concentrations of urea and ammonium lactate and is aimed at cleansing and conditioning of hair and skin, and not for the treatment of diseased or compromised skin.
The prior art therefore teaches either compositions that comprise high concentrations of urea or ammonium lactate, which, as is discussed hereinabove, suffer severe limitations and hence are disadvantageous, or compositions that comprise a combination of urea and ammonium lactate, whereby these substances are used in relatively low concentrations and therefore do not serve as efficient active ingredients for treating dry skin and scalp conditions.

Method used

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  • Topical compositions of urea and ammonium lactate
  • Topical compositions of urea and ammonium lactate
  • Topical compositions of urea and ammonium lactate

Examples

Experimental program
Comparison scheme
Effect test

example 1

Skin and Scalp Compositions

[0211] Representative examples of skin and scalp topical compositions, according to the present invention, were prepared in various forms using conventional methods (see, for example, Harry's Cosmeticology, Seventh Edition, Edited by JB Wilkinson and R J Moore, Longmann Scientific & Technical, 1982, Chapter 13 “The Manufacture of Cosmetics” pages 757-799), whereby each of these representative compositions comprise 20 weight percentages (% wt.) urea and 12 weight percentages of ammonium lactate, obtained using 17 weight percentages of a 70% ammonium lactate source solution. The components of each of these compositions are listed hereinbelow:

[0212] Composition 1—A Skin Foam:

GLYCERINE2.0% wt.ALLANTOIN0.2% wt.UREA USP 20% wt.CETYL ALCOHOL0.5% wt.VASELINE ™8.0% wt.Isopropyl myristate4.0% wt.MYRITOL 318 ™3.0% wt.TWEEN 60 ™1.0% wt.SILICON D.C.350 ™0.5% wt.VIT.E ACETATE0.1% wt.MONTANOV 68 ™1.5% wt.PHENONIP ™0.7% wt.AMYLUM RICE STARCH ™2.0% wt.PURASAL NH 70 ™* ...

example 2

Comparative Activity Tests

[0221] The activity of the compositions of the present invention in the treatment of dry skin was tested and compared with that of a commercially available dry skin product, containing ammonium lactate only. Thus, a skin foam composition that comprises 20% urea and 12% ammonium lactate (Composition 1 hereinabove) was tested for its activity in the treatment of dry skin according to the protocol described hereinbelow, whereby an Ammonium Lactate 12% cream, marketed by Clay Park Ltd., served as control.

[0222] Protocol: The study subjects were healthy volunteers, apparently free of diseases, aged 18 to 65, and having dry skin. The subjects had no history of skin or topical diseases and had no known sensitivity to any of the tested substances or to other components in the tested compositions.

[0223] Each volunteer was assigned a serial number by ISR.

[0224] Six volunteers that suffered from dry skin applied the tested preparations twice a day, on a daily basi...

example 3

Comparative Activity Tests

[0238] The activity of the compositions of the present invention in the treatment of dry skin was tested and compared with that of a commercially available dry skin product, containing urea only. Thus, a cream composition that comprises 20 weight percentages urea and 12 weight percentages ammonium lactate (Composition 4 hereinabove, also referred to herein as Moisturizing Complex Cream or MCC) was tested for its activity in the treatment of dry skin according to the protocol described hereinbelow, whereby an Urea 40% cream, marketed by Doak Dermatologics, a subsidiary of Bradley Pharmaceuticals Inc. (also referred to herein as Urea Cream or UC), served as control.

[0239] Protocol:

[0240] Fifteen (15) healthy volunteers, free of disease, aged 18 to 65, suffering from dry skin (xerosis) participated in this study.

[0241] The study consisted of a 14-days (two-weeks) treatment period in which a composition of the present invention (Composition 4, MCC) was appl...

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Abstract

Pharmaceutical, cosmetic and cosmeceutical compositions for topical application, containing, as active ingredients, urea and / or derivatives thereof and alpha-hydroxy acid and / or an ammonium salt thereof, such as ammonium lactate, processes of manufacturing same and use of same in the treatment of medical and cosmetic skin and scalp conditions.

Description

RELATED APPLICATIONS [0001] This application is a continuation of U.S. patent application Ser. No. 10 / 850,461 filed May 21, 2004, which claims the benefit of U.S. Provisional Patent Applications Nos. 60 / 494,579 filed Aug. 13, 2003, 60 / 494,581 filed Aug. 13, 2003, 60 / 510,554 filed Oct. 14, 2003 and 60 / 527,279 filed Dec. 8, 2003, the contents of which are hereby incorporated by reference in their entirety.FIELD AND BACKGROUND OF THE INVENTION [0002] The present invention relates to novel pharmaceutical, cosmetic and cosmeceutical compositions for topical application, and their use in the treatment of medical, cosmetic and cosmeceutical conditions such as dry skin and / or scalp. [0003] Dry skin is a common condition associated with a plurality of disorders and frequently requires therapeutic intervention. [0004] Dermatologists often call dry skin in later life “xerosis” or “ichthyosis”. Xerosis is a term used to describe abnormal skin dryness. Ichthyosis is a term used to described a gr...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/19A61P17/00A61K8/365A61K8/42A61K9/12A61K31/17A61K47/00A61K47/12A61Q5/00A61Q19/00
CPCA61K8/365A61K8/42A61K9/0014A61K9/122A61K31/17A61K31/19A61K47/12A61Q19/007A61Q19/00A61Q5/006A61K2300/00A61P17/00
Inventor ARKIN, MOSHEAVRAM, NIRBURIAKOVSKY, OLGAZEEVI, AMIRASCHNEIDER, BENJAMINCHERKEZ, STEPHENNIVY, STELLA
Owner AGIS INDUSTRIES (1983) LTD
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